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Quantitative Proteomics Reveals Cellular Off-Targets of a DDR1 Inhibitor
Xu,Jiaqian1,2; Zhang,Zhang1; Lin,Ligen3; Sun,Hongyan2; White,Lorenzo V.1; Ding,Ke1; Li,Zhengqiu1
Source PublicationACS Medicinal Chemistry Letters

Target identification of small molecules is a great challenge but an essential step in drug discovery. Here, a quantitative proteomics approach has been used to characterize the cellular targets of DR, a DDR1 inhibitor. By taking advantage of competitive affinity-based protein profiling coupled with bioimaging, Cathepsin D (CTSD) was found to be the principle off-target of DR in human cancer cells. Further findings suggest the potential of DR as a novel CTSD inhibitor for breast cancer treatment. In addition, a trans-cyclooctene (TCO) containing probe was developed to track the binding between DR and its target proteins in living systems and could be a useful tool for DDR1 detection.

KeywordBioimaging Chemoproteomics Ddr1 Photoaffinity Labeling Target Identification
URLView the original
Indexed BySCIE ; IC
WOS Research AreaPharmacology & Pharmacy
WOS SubjectChemistry, Medicinal
WOS IDWOS:000526402700021
Scopus ID2-s2.0-85080126008
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Cited Times [WOS]:6   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Corresponding AuthorLin,Ligen; Ding,Ke; Li,Zhengqiu
Affiliation1.Intl. Coop. Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development,Ministry of Education (MOE) of China,Guangzhou Key Laboratory of Precision Chemical Drug Development,School of Pharmacy,Jinan University
2.Department of Chemistry,City University of Hong Kong,Hong Kong,83 Tat Chee Avenue,SAR 999077,Hong Kong
3.State Key Laboratory of Quality Research in Chinese Medicine,Institute of Chinese Medical Sciences,University of Macau,Taipa,Macao
Corresponding Author AffilicationInstitute of Chinese Medical Sciences
Recommended Citation
GB/T 7714
Xu,Jiaqian,Zhang,Zhang,Lin,Ligen,et al. Quantitative Proteomics Reveals Cellular Off-Targets of a DDR1 Inhibitor[J]. ACS Medicinal Chemistry Letters,2020,11(4):535-540.
APA Xu,Jiaqian,Zhang,Zhang,Lin,Ligen,Sun,Hongyan,White,Lorenzo V.,Ding,Ke,&Li,Zhengqiu.(2020).Quantitative Proteomics Reveals Cellular Off-Targets of a DDR1 Inhibitor.ACS Medicinal Chemistry Letters,11(4),535-540.
MLA Xu,Jiaqian,et al."Quantitative Proteomics Reveals Cellular Off-Targets of a DDR1 Inhibitor".ACS Medicinal Chemistry Letters 11.4(2020):535-540.
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